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United States Patent | 5,250,564 |
Hirschmann ,   et al. | October 5, 1993 |
Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.
Inventors: | Hirschmann; Ralph (Blue Bell, PA); Leahy; Ellen (Philadelphia, PA); Sprengeler; Paul (Philadelphia, PA) |
Assignee: | Trustees of the University of Pennsylvania (Philadelphia, PA) |
Appl. No.: | 806048 |
Filed: | December 12, 1991 |
Current U.S. Class: | 514/414; 514/415; 548/455; 548/469 |
Intern'l Class: | A61K 031/40; A61K 031/405; C07D 209/04 |
Field of Search: | 548/455,469 514/414,415 |
Foreign Patent Documents | |||
89122396.8 | Jun., 1990 | EP. |
Sherman and Spatola, J. Am. Chem. Soc., 112, 1990, 433. Veber and Hirschmann, et al., Proc. Natl. Acad. Sci. USA, 1978 75 2636. Thorsett, et al., Biochem. Biophys. Res. Comm., 1983 111 166. Veber and Hirschmann, et al., Life Sciences, 1984, 34, 1371. Veber and Hirschmann, et al., Nature, 1981, 292. Raynor and Reisine, Journal of Pharmacology and Experimental Therapeutics, 1989, 251;2, 510. Reisine, et al., Brain Research, 1979, 177, 241. |
TABLE 1 ______________________________________ CH.sub.3 HOCH.sub.2 C.sub.6 H.sub.5CH.sub.2 HOC.sub.6 H.sub.5CH.sub.2 ##STR5## ##STR6## ##STR7## HSCH.sub.2 HO.sub.2 CCH(NH.sub.2)CH.sub.2SSCH.sub.2 CH.sub.3CH.sub.2 CH.sub.3SCH.sub.2CH.sub.2 CH.sub.3CH.sub.2SCH.sub.2CH.sub.2HOCH.sub.2CH.sub.2 HO.sub.2 CCH.sub.2CH.sub.2 ##STR8## HCO.sub.2CH.sub.2CH.sub.2 NH.sub.2 C(O)CH.sub.2CH.sub.2 (CH.sub.3).sub.2CH (CH.sub.3).sub.2CHCH.sub.2 CH.sub.3CH.sub.2CH.sub.2 H.sub.2 NCH.sub.2CH.sub.2CH.sub.2 H.sub.2 NC(NH)NHCH.sub.2CH.sub.2CH.sub.2 H.sub.2 NC(O)NHCH.sub.2CH.sub.2CH.sub.2 CH.sub.3CH.sub.2CH(CH.sub.3) CH.sub.3CH.sub.2CH.sub.2CH.sub.2 H.sub.2 NCH.sub.2CH.sub.2CH.sub.2CH.sub.2 ______________________________________